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Table 3 Urine pharmacokinetic variables of lucerastat

From: Lucerastat, an iminosugar with potential as substrate reduction therapy for glycolipid storage disorders: safety, tolerability, and pharmacokinetics in healthy subjects

Study

Dose regimen

 

Ae 0-12h [21]

Ae 12-24h [21]

Ae 0-24h [21]

% of dose

SAD

100 mg

 

47 (21)

6 (4)

53 (24)

53 (24)

300 mg

 

145 (52)

10 (6)

153 (54)

49 (20)

500 mg

 

256 (24)

24 (12)

280 (12)

56 (6)

1000 mg

 

452 (122)

49 (46)

501 (98)

50 (10)

2x1000 mg

 

524 (50)

304 (191)

904 (295)

45 (15)

MAD

200 mg

Day 7

160 (14)

145 (31)

305 (40)

76 (10)

500 mg

Day 7

357 (64)

362 (56)

719 (101)

72 (10)

1000 mg

Day 7

864 (243)

830 (152)

1695 (289)

85 (15)

  1. Data are arithmetic means (standard deviation); Ae cumulative amount of unchanged drug excreted in urine, SAD single ascending dose, MAD multiple ascending dose